Antispasmodic effect of Jatropha gossypiifolia is mediated through dual blockade of muscarinic receptors and Ca2+ channels

Abstract

Abstract:The antispasmodic activity of Jatropha gossypiifolia L., Euphorbiaceae, aerial parts was investigated in rodents using the mouse intestinal transit model and acetylcholine (ACh, to 10 -4 M) and calcium (CaCl 2 , 10 -4 to 10 -1 M)-induced contractions of isolated rat jejunum. Similar to atropine (1 mg/kg), oral doses of ethanolic extract (EE) of J. gossypiifolia (500, 1000 and 2000 mg/kg) produced a decrease in intestinal transit (37.6 to 57.1%) when compared with control. The ACh-induced contraction in the jejunum was inhibited by EE (0.5, 1.0 and 2.0 mg/ mL), chloroformic (CF) and aqueous fractions (0.1 and 0.5 mg/mL) and methanolic subfraction (0.05 and 0.25 mg/mL), suggesting an antimuscarinic mechanism. CaCl 2 -induced responses in jejunum were also attenuated in the presence of CF (0.05 and 0.1 mg/mL) implying a direct interference of CF with the influx of calcium ions in the cells. Only the organic fraction of the extract had a calcium-antagonist effect, whereas both chloroformic and aqueous fractions had anticholinergic effect. These results suggest that the antispasmodic effect of J. gossypiifolia may be due a combination of anticholinergic and calcium antagonist mechanisms.

Effects of Jatropha gossypiifolia L. on the blood pressure and vascular reactivity of rats

“…These initial results were in agreement with the dates observed by several authors that showed that ethanolic extract and fractions of J. gossypiifolia L. antagonized, competitive and non-competitive manner, NA or CaCl 2 -induced contractile responses, as well as others stimulus in vascular and non-vascular smooth muscle from normotensive rats (Abreu et al, 2003;Silva et al, 2011;Paes et al, 2012), no however, formed a complex with calcium ions (Abreu et al, 2002). Other studies also shows that compounds isolated from Jatropha genus plants inhibited the contractions induced by several agonist in heart muscle or vascular and non-vascular smooth muscle from rats, guinea pigs and rabbits (Ojewole and Odebiyi, 1981;Calixto and Sant'ana, 1987;Trebien et al, 1988).…”

“…After this process, the EEJg was fractioned using chloroform and water as solvent, obtaining the aqueous (AFJg) and chloroformic (CFJg) fractions, with a yield of 71 and 29%, respectively (Abreu et al, 2003;Silva et al, 2011).…”

“…This alkaloid also inhibits the contractile responses induced by electrical stimulation or by noradrenaline (NA) in vascular and non-vascular smooth muscle from rats, guinea pigs and rabbits (Ojewole and Odebiyi, 1981). Silva et al (2011) have investigated the effect of J. gossypiifolia L. aerial parts on intestinal transit velocity and on isolated. It was observed that the chloroformic fraction of J. gossypiifolia L. ethanolic extract had a calcium-antagonist effect, whereas both chloroformic and aqueous fractions had anticholinergic effect, suggesting that the antispasmodic effect of J. gossypiifolia L. may be due to a combination of anticholinergic and calciumantagonist mechanisms.…”

Jatropha gossypiifoliaL. (Euphorbiaceae): A Review of Traditional Uses, Phytochemistry, Pharmacology, and Toxicology of This Medicinal Plant

“…Aiming to determine the possible action mechanism of J. gossypiifolia aerial parts ethanol extract as antidiarrheal agent, Silva et al [ 119 ] have investigated the effect of this extract on intestinal transit velocity and on isolated rat jejunum. At 500, 1000, and 2000 mg/kg, by oral route in mice, the extract showed significant antispasmodic activity in mouse intestinal transit model when compared to control.…”

“…At 0.5, 1.0, and 2.0 mg/mL, the crude extract inhibited in vitro the acetylcholine and calcium-induced contractions of isolated rat jejunum. The chloroform and aqueous fractions were obtained and it was observed that only the chloroform fraction of the extract had a calcium-antagonist effect, whereas both chloroformic and aqueous fractions had anticholinergic effect, suggesting that the antispasmodic effect of J. gossypiifolia may be due to a combination of anticholinergic and calcium-antagonist mechanisms [ 119 ].…”